Gefapixant
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MedKoo CAT#: 561852

CAS#: 1015787-98-0

Description: Gefapixant, also known as AF-219 or MK-7264, is a P2X3 receptor antagonist. Gefapixant is currently under clinical trials for chronic cough. It is believed that excessive activation of P2X3 receptors is associated with hyper-sensitization of sensory neurons. Neuronal hyper-sensitization in the airways and lungs, triggered by injury or infection, can cause an exaggerated, persistent and frequent urge to cough, so called chronic cough. P2X3 receptors seem to have a key role in mediation of cough neuronal hypersensitivity. Antagonists of P2X3 receptors such as AF-219 are a promising new group of antitussives.


Price and Availability

Size
Price

25mg
USD 250
200mg
USD 1450
2g
USD 5250
Size
Price

50mg
USD 450
500mg
USD 2450
Size
Price

100mg
USD 850
1g
USD 3450

Gefapixant, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 561852
Name: Gefapixant
CAS#: 1015787-98-0
Chemical Formula: C14H19N5O4S
Exact Mass: 353.1158
Molecular Weight: 353.39
Elemental Analysis: C, 47.58; H, 5.42; N, 19.82; O, 18.11; S, 9.07


Synonym: Gefapixant; MK-7264; MK 7264; MK7264; AF-219; AF219; AF 219; RO4926219; RO-4926219; RO 4926219;

IUPAC/Chemical Name: 5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide

InChi Key: HLWURFKMDLAKOD-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H19N5O4S/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19)

SMILES Code: O=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
2934.99.90.01


References

1: Wang J, Wang Y, Cui WW, Huang Y, Yang Y, Liu Y, Zhao WS, Cheng XY, Sun WS, Cao P, Zhu MX, Wang R, Hattori M, Yu Y. Druggable negative allosteric site of P2X3 receptors. Proc Natl Acad Sci U S A. 2018 May 8;115(19):4939-4944. doi: 10.1073/pnas.1800907115. Epub 2018 Apr 19. PubMed PMID: 29674445; PubMed Central PMCID: PMC5948998.

2: Burnstock G. The therapeutic potential of purinergic signalling. Biochem Pharmacol. 2018 May;151:157-165. doi: 10.1016/j.bcp.2017.07.016. Epub 2017 Jul 21. Review. PubMed PMID: 28735873.

3: Sheridan C. Merck stakes out 'irritable' neuron territory with $1.25 billion. Nat Biotechnol. 2016 Sep 8;34(9):900. doi: 10.1038/nbt0916-900. PubMed PMID: 27606448.

4: Abdulqawi R, Dockry R, Holt K, Layton G, McCarthy BG, Ford AP, Smith JA. P2X3 receptor antagonist (AF-219) in refractory chronic cough: a randomised, double-blind, placebo-controlled phase 2 study. Lancet. 2015 Mar 28;385(9974):1198-205. doi: 10.1016/S0140-6736(14)61255-1. Epub 2014 Nov 25. PubMed PMID: 25467586.

5: Morice AH. Developing antitussives the clinician's pipeline-what do we need? J Thorac Dis. 2014 Oct;6(Suppl 7):S735-8. doi: 10.3978/j.issn.2072-1439.2014.08.40. Review. PubMed PMID: 25383208; PubMed Central PMCID: PMC4222922.

6: Ochoa-Cortes F, Liñán-Rico A, Jacobson KA, Christofi FL. Potential for developing purinergic drugs for gastrointestinal diseases. Inflamm Bowel Dis. 2014 Jul;20(7):1259-87. doi: 10.1097/MIB.0000000000000047. Review. PubMed PMID: 24859298; PubMed Central PMCID: PMC4340257.

7: Ford AP, Undem BJ. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013 Dec 19;7:267. doi: 10.3389/fncel.2013.00267. Review. PubMed PMID: 24391544; PubMed Central PMCID: PMC3867694.